内皮素及其受体拮抗剂与心血管疾病关系的研究进展

Recent Progress on Endothelin/Endothelin Receptor Antagonists and Cardiovascular Diseases

内皮素通过激活内皮素受体发挥缩血管和促血管平滑肌增殖的作用,在心血管疾病的发生发展中起重要作用。如今,内皮素受体拮抗剂已应用于肺动脉高压的临床治疗。现已证实,心力衰竭患者在应用标准抗心力衰竭治疗基础上应用内皮素受体拮抗剂是无益的。在动物模型和高血压患者中选择性和非选择性的内皮素受体拮抗剂都可降低血压,且评估其有效性和安全性的临床试验正在进行,也许将来高血压、冠心病等疾病将成为内皮素受体拮抗剂的适应证。

Endothelin induces vasoconstriction and vascular smooth muscle cell proliferation through activating endothelin receptor, thus plays important roles in the development of cardiovascular disease. Today, endothelin receptor antagonist has become reality in clinical application for the treatment of pulmonary hypertension, It has been confirmed that endothelin receptor antagonist doesn＇t benefit for heart failure when giving standard anti-heart failure therapy. Both selective and dual-acting endothelin receptor antagonists can reduce systemic blood pressure in animal models and in hypertensive patients,clinical trials evaluating the efficacy and safety of these agents are underway. Possible future indications may include hypertension, coronary artery disease and so on.